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Identification of novel and improved antimitotic agents derived from noscapine. | LitMetric

AI Article Synopsis

  • Researchers synthesized analogues of noscapine to test their potential as cancer-fighting agents.
  • A new method for O-demethylation allowed for the creation of a specific compound, aniline 6, which stops cancer cells in the G2/M phase of their growth cycle.
  • Aniline 6 is effective at very low concentrations and is significantly more potent than noscapine, making it a promising candidate for cancer treatment.

Article Abstract

Analogues of the natural product noscapine were synthesized and their potential as antitumor agents evaluated. The discovery of a novel regioselective O-demethylation facilitated the synthesis of the potent aniline 6, which arrests mammalian cells in the G2/M phase of the cell cycle at 0.1 microM and also affects tubulin polymerization. Aniline 6 is orally bioavailable and is 250-fold more potent than noscapine in reducing cell proliferation in rapidly dividing cells.

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Source
http://dx.doi.org/10.1021/jm050674qDOI Listing

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